An inhibitor of PAK4
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PF-3758309

Item No. 19186

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1S)-2-(dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide
CAS Number
898044-15-0
Synonyms
  • PF-309
Molecular Formula
C25H30N8OS
Formula Weight
490.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/ml
λmax
266, 312 nm
SMILES
CN(C)C[C@@H](NC(N1CC(C(NC2=NC(C)=NC3=C2SC=C3)=NN4)=C4C1(C)C)=O)C5=CC=CC=C5
InChi Code
InChI=1S/C25H30N8OS/c1-15-26-18-11-12-35-20(18)23(27-15)29-22-17-13-33(25(2,3)21(17)30-31-22)24(34)28-19(14-32(4)5)16-9-7-6-8-10-16/h6-12,19H,13-14H2,1-5H3,(H,28,34)(H2,26,27,29,30,31)/t19-/m1/s1
InChi Key
AYCPARAPKDAOEN-LJQANCHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

    $115

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    25 mg

    $263

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    Product Description

    PF-3758309 is an ATP-competitive inhibitor of PAK4, preventing the phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and blocking anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM).1 It also inhibits the ability of kinase domains from other PAKs to phosphorylate peptide substrates (Kis = 18.1, 17.1, 13.7, 190, and 99 nM for PAKs 5, 6, 1, 2, and 3, respectively).1 PF-3758309 blocks the growth of multiple human tumor xenografts.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Murray, B.W., Guo, C., Piraino, J., et al. Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proc. Natl. Acad. Sci. USA 107(20), 9446-9451 (2010).